In this study we describe a new theranostic nanostytem to combine those functions together. GX1, the peptide identified by phage display technology, is a tumor vasculature endothelium specific ligand. Endostar, a novel recombinant human endostatin, has been proved to inhibit tumor angiogenesis. In this study, Endostar-loaded PLA nanoparticles (EPNPs) were first prepared, and then GX1 was coupled to the surface of EPNPs for targeting therapy, last a near infrared (NIR) dye IRDye 800CW was conjugated to the surface of EPNPs for monitoring the biodistributon. This GX1-EPNPs-NIR dye IRDye 800CW (GEN) multifunction drug delivery system not only facilitates efficient delivery of chemotherapeutic agents to tumor site, while minimizing systemic toxicity and side effects, but also enables to real time monitor tumor targeting in vivo. Compare to the Endostar and EPNPs, the GEN inhibited the subcutaneous colon tumor more obviously both in tumor volume and bioluminescence imaging (BLI) light intensity during the 10 days drug treatment.